SYNTHESIS AND ANTI-TUMOR ACTIVITIES OF 1,4-BIS［3- (AMINO-DITHIOCARBOXY)PROPIONYL］ PIPERAZINE DERIVATIVES

目的寻找并合成低毒、有较强抗肿瘤活性的哌嗪类化合物。方法和结果以1,4-二(3-溴丙酰基)哌嗪为先导物，合成了一系列1,4-二［3-(氨基硫代甲酰硫基)丙酰基］哌嗪类新化合物，并测试了这些化合物(4a-j)对8种瘤细胞株的体外抗肿瘤活性。结论体外抗肿瘤活性试验结果表明，大多数化合物显示一定的抗肿瘤活性，尤其是化合物4c，4d和4e，浓度在10 μmol.L-1时，对HL-60细胞抑制率分别为44%，90%和70%。AIM To synthesize piperazine derivatives and screen anti-tumor compounds with higher activity and lower toxicity. METHODS Selecting 1,4-bis(3-bromopropionyl)piperazine as leading compound, a series of 1,4-bis［3-(amino-dithiocarboxy)propionyl］ piperazine derivatives (4a-j) were synthesized through the use of aminodithiocarboxylate. All the synthetic compounds (4a-j) were tested for their anti-tumor activity against eight kinds of tumor cells. RESULTS Compounds (4a-j) are new compounds, among them, compounds 4c, 4d and 4e showed anti-tumor activity against HL-60. The inhibition of compounds 4c, 4d and 4e against HL-60 are 44%, 90% and 70% respectively, at the concentration of 10 μmol.L-1. However, the inhibition of the other kinds of anti-tumor cells are not distinctive. CONCLUSION These results suggest that this may be one of the effective routes to improve the anti-tumor activity and reduce the toxicity of 1,4-bis(3-bromopropionyl)piperazine.PubMed中文核心期刊要目总览(PKU)中国科学引文数据库(CSCD)03185-1873